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    • 92. 发明授权
    • 18-membered nitrobenzyl- and aminobenzyl-substituted cyclohexadepsipeptides for controlling endoparasites and a process for their preparation
    • 用于控制内寄生虫的18元硝基苄基 - 和氨基苄基取代的环己缩肽及其制备方法
    • US07645738B2
    • 2010-01-12
    • US10582555
    • 2004-12-07
    • Peter JeschkeAchim Harder
    • Peter JeschkeAchim Harder
    • A61K38/00
    • C07K11/02A61K38/00C07D273/00
    • The invention relates to cyclic depsipeptides, especially 18-membered cyclohexadepsipeptides of general formula (I) and the salts thereof, wherein R1 represents nitrobenzyl or R′R″N-benzyl—wherein R′ and R″ independently represent hydrogen, optionally substituted C1-C4-alkyl, formyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxycarbonyl, or hydroxy-C1-C2-alkyl-sulfonyl-C1-C2-alkyl, or, together with the nitrogen atom to which they are bound, R′ and R″ form an optionally substituted monocyclic or polycyclic, optionally bridged and/or spirocyclic, saturated or unsaturated heterocycle containing between one and three other heteroatoms from the group of nitrogen, oxygen and sulphur, or R′ and R″ together form C3-C5-alkylene monocarbonyl or an optionally substituted diacyl radical of a C4-C6-dicarboxylic acid—and R2, R3 and R4 independently represent C1-C4-alkyl. The invention also relates to the optical isomers and racemates of said cyclic depsipeptides, to a method for the production thereof, and to the use of the same for controlling endoparasites.
    • 本发明涉及环状缩肽,特别是通式(I)的18元环己缩肽和其盐,其中R1表示硝基苄基或R'R''N-苄基,其中R'和R“独立地表示氢,任选取代 C 1 -C 4烷基,甲酰基,C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基羰基或羟基-C 1 -C 2 - 烷基 - 磺酰基-C 1 -C 2烷基,或与氮原子一起 R'和R“形成任选取代的单环或多环,任选桥连和/或螺环,饱和或不饱和的杂环,其含有来自氮,氧和硫的一个和三个其它杂原子,或R '和R'一起形成C 3 -C 5 - 亚烷基单羰基或C 4 -C 6 - 二羧酸的任选取代的二酰基 - ,并且R 2,R 3和R 4独立地表示C 1 -C 4 - 烷基。 本发明还涉及所述环状缩酚酸酯的光学异构体和外消旋体,其制备方法及其用于控制​​内寄生虫的用途。
    • 100. 发明授权
    • Use of cyclic depsipeptides having 12 ring atoms for combating
endoparasites, new cyclic despipeptides having 12 ring atoms, and
processes for their preparation
    • 具有12个环原子的环状缩水甘油醚与具有12个环原子的新环状脱磷酸酯的反应的内源寄生虫的使用及其制备方法
    • US5663140A
    • 1997-09-02
    • US372543
    • 1995-01-13
    • Jurgen ScherkenbeckPeter JeschkeAndrew PlantAchim HarderNorbert Mencke
    • Jurgen ScherkenbeckPeter JeschkeAndrew PlantAchim HarderNorbert Mencke
    • A61K31/33A61K31/38A61K31/41A61K38/00A61P33/00A61P33/10C07D273/00C07D273/08C07D413/06C07K11/02A61K35/78
    • C07D273/00A61K31/33A61K31/38C07D413/06
    • The present invention relates to the use of cyclic depsipeptides having 12 ring atoms of the general formula (I) ##STR1## in which R.sup.1 and R.sup.4 independently of one another represent hydrogen, straight-chain or branched alkyl, cycloalkyl, aralkyl, aryl, heteroaryl or heteroarylalkyl, each of which is optionally substituted,R.sup.2, R.sup.3, R.sup.5 and R.sup.6 independently of one another represent hydrogen, straight-chain or branched alkyl having up to 8 carbon atoms, halogenoalkyl, hydroxyalkyl, alkanoyloxyalkyl, alkoxyalkyl, aryloxyalkyl, mercaptoalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, carboxyalkyl, alkoxycarbonylalkyl, arylalkoxycarbonylalkyl, carbamoylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, guanidinoalkyl which can optionally be substituted by one or two benzyloxycarbonyl radicals or by one, two, three or four alkyl radicals, alkoxycarbonylaminoalkyl, 9-fluorenylmethoxycarbonyl(Fmoc)aminoalkyl, alkenyl, cycloalkyl, cycloalkylalkyl, and optionally substituted aryl, arylalkyl, heteroaryl and heteroarylalkyl, and their optical isomers and racemates,in medicine and veterinary medicine for combating endoparasites, to new depsipeptides having 12 ring atoms, and to processes for their preparation.
    • 本发明涉及具有通式(I)的12个环原子的环状缩水甘油酯的用途,其中R 1和R 4彼此独立地表示氢,直链或支链烷基,环烷基,芳烷基, 芳基,杂芳基或杂芳基烷基,其各自任选被取代,R 2,R 3,R 5和R 6彼此独立地表示氢,具有至多8个碳原子的直链或支链烷基,卤代烷基,羟烷基,烷酰氧基烷基,烷氧基烷基,芳氧基烷基, 烷基磺酰基烷基,烷基亚磺酰基烷基,烷基磺酰基烷基,羧基烷基,烷氧基羰基烷基,芳基烷氧基羰基烷基,氨基甲酰基烷基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,胍基烷基,其可以任选被一个或两个苄氧基羰基取代或被一个,二个,三个或四个烷基取代,烷氧基羰基氨基烷基, 芴基甲氧基羰基(Fmoc)氨基烷基,烯基,环烷基,环烷基烷基和任选取代的a 芳基烷基,杂芳基和杂芳基烷基,以及它们的光学异构体和外消旋体,在用于抗内寄生物的医药和兽医学中,具有12个环原子的新的缩肽,以及它们的制备方法。